1. Field of the Invention
The present invention relates to new 6-hydroxy and 6-oxo-androstane derivatives and to pharmaceutical compositions containing same for the treatment of cardiovascular disorders such as heart failure and hypertension.
2. Summary of the Invention
The compounds of the invention have the following general formula (I): ##STR2## wherein: the symbol A represents CH--OR, C.dbd.N--OR, CH--CH.dbd.N--OR and C.dbd.CH--CH.dbd.N--OR,
where:
R represents a C2-C6 alkyl group substituted by NR.sup.3 R.sup.4, NHC(NH)NHR.sup.5, C(NH)NR.sup.6 R.sup.7 or --O--(C2-C4-alkyl)-NR.sup.3 R.sup.4 groups, PA1 R.sup.1 represents H, C1-C4 lower alkyl and C2-C6 acyl groups; PA1 R.sup.2 represents H, methyl, C2-C6 alkyl group unsubstituted or substituted by NR.sup.3 R.sup.4, C2-C6 acyl groups, benzoyl, benzoyl substituted by one or more hydroxy, methoxy, amino, chloro, fluoro, methylmercapto groups.
wherein R.sup.3 and R.sup.4, which may be the same or different, are H. C1-C6 lower alkyl group, benzyl or phenyl or R.sup.3 and R.sup.4, taken together with the nitrogen atom, form an unsubstituted or substituted saturated or unsaturated mono-heterocyclic 5- or 6-membered ring optionally containing another heteroatom chosen from oxygen, sulphur or nitrogen, PA2 R.sup.5, R.sup.6 and R.sup.7, which are the same or different, may be H or C1-C4 lower alkyl;
the symbol ------. in position 6 and in position 17 represents independently a single or a double bond;
when the symbol ------. represents a single bond
when the symbol ------. represent a double bond, it means a keto group and no R.sup.1 or R.sup.2 is present.
The invention includes within its scope all the possible stereoisomers, in particular Z and E isomers and syn and anti isomers, optical isomers and their mixtures of the compounds of formula (I).
Also included in this invention are pharmaceutically acceptable salts of (I), which retain the biological activity of the base and are derived from known acids such as, for example, hydrochloric, sulphuric, phosphoric, malic, tartaric, maleic, citric, methanesulfonic, benzoic acid or other acids used in the art.